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A rapid,accurate,and sensitive analytical method,ultrasonication-assisted spraying based fine droplet formation-liquid phase microextraction-gas chromatography-mass spectrometry (UA-SFDF-LPME-GC-MS),was proposed for the determination of trace amounts of hydroxychloroquine sulfate in human serum,urine,and saliva samples.To determine the best extraction strategy,several liquid and solid phase extraction methods were investigated for their efficiencies in isolation and preconcentration of hydroxychloroquine sulfate from biological matrices.The UA-SFDF-LPME method was determined to be the best extraction method as it was operationally simple and provided accurate results.Variables such as the extraction solvent,spraying number,sodium hydroxide concentration and volume,sample vol-ume,mixing method,and mixing period were optimized for the proposed method using the one-variable-at-a-time approach.In addition,Tukey's method based on a post hoc comparison test was employed to evaluate the significant difference between the parameters inspected.After the optimiza-tion studies,the limit of detection (LOD) and limit of quantification (LOQ) were determined to be 0.7 and 2.4 μg/kg,respectively.The sensitivity of the GC-MS system based on the LOD was enhanced approxi-mately 440-fold when the UA-SFDF-LPME method was employed.Spiking experiments were also con-ducted for the human serum,urine,and saliva samples to determine the applicability and accuracy of the proposed method.Recoveries for the human serum,urine,and saliva samples were found to be in the ranges of 93.9％-101.7％,95.2％-105.0％,and 93.1％-102.3％,respectively.These results were satisfactory and indicated that the hydroxychloroquine sulfate level in the above biological samples could be analyzed using the proposed method.
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Objective To establish an online quantitative analysis model for moisture content assay of hydroxychloroquine sulfate particles by near infrared (NIR) spectroscopy. Methods The NIR spectra were collected in real time when the material particles were dried in the fluidized bed. Meanwhile the water content of the particles was measured with the standard moisture tester. The multiplicative signal correction (MSC) and first derivative followed by Karl Norris smoothing were used for spectra pretreatment. Two spectral range (4 935−5 336 cm−1 and 6 911−7 297 cm−1) were selected for the quantitative model with the partial least squares (PLS) regression. Results The quantitative calibration model had good correlation coefficients with Rc value=0.952 9 and Rp value=0.936 6. The root mean square error of calibration (RMSEC) was 0.408 and the root mean square error of prediction error (RMSEP) was 0.435. The ratio of standard deviation of validation set to prediction standard deviation (RPD) was 5.18. There was no significant difference between the predicted value and the reference value by t test when the established model was applied in large-scale production. Conclusion The online model established for monitoring water content has high accuracy and stability, which can be applied in industrial scale process to monitor the particle moisture in real time.
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Objective:To observe the effect of modified Yiweitang on fatigue symptom and immunological indicators in primary Sjörgren′s Syndrome (pSS). Method:By random, control, single-blind method, 116 cases of patients with pSS were divided into treatment group and control group, with 58 cases in each group. The treatment group was given modified Yiweitang, a dose a day, twice a day， and the control group was given hydroxychloroquine sulfate (HCQ) 200 mg/time, twice a day. The treatment lasted for six months. Visual analogue scale (VAS) of fatigue symptoms, total traditional Chinese medicine (TCM) syndrome score, TCM fatigue score, rheumatoid factor (RF) and serum immunoglobulin G (IgG) were used to compare two groups before and after treatment. Result:After treatment, the treatment group had a better efficacy on TCM syndromes than control group (Z=3.712, P<0.05). After treatment, the treatment group were superior to control group in improvement of TCM fatigue score and VAS score of fatigue symptom (P<0.05). After 6 months of treatment, IgG level in treatment group decreased significantly compared with before treatment, with statistical differences (P<0.05), but no difference between treatment group and control group. After treatment, RF in two groups showed no significant decrease compared with before treatment. The incidence of adverse reactions in the treatment group and the control group were 1.75%（1/57） and 25.49%（13/51）, respectively. Conclusion:Compared with HCQ, modified Yiweitang can significantly alleviate fatigue and overall symptoms of patients of pSS, both of which can reduce serum IgG, and the efficacy of modified Yiweitang is more obvious than hydroxychloroquine sulfate. Both drugs had no significant effect on RF level of pSS patients. After long-term administration, modified Yiweitang is safer than hydroxychloroquine sulfate in the treatment of pSS.
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A novel coronavirus disease (COVID-19) was identified in Wuhan City, Hubei Province of China by the end of 2019, and then, the disease spread across China and became a global pandemic. Nevertheless, there are no effective treatments or vaccines for COVID-19 until now. In addition to the treatment of patients with COVID-19, the China Medical Treatment Expert Group for COVID-19 is active to study and screen effective antiviral drugs, and has found that chloroquine, an old antimalarial,shows activity against SARS-CoV-2. Then, chloroquine was included in the Guidelines for the Diagnosis and Treatment of COVID-19 in China (version 6) issued by National Health Commission of the People’s Republic of China. Currently, chloroquine phosphate and hydroxychloroquine sulfate, two chloroquine derivatives, are under clinical use. Although these two agents exhibit similar mechanisms of drug actions, there is a difference between these two chemicals in terms of target populations, therapeutic efficacy and adverse reactions. This paper summarizes the currently available data and experiences from clinical treatment for malaria with chloroquine drugs, so as to provide insights into the more rational use of chloroquine agents for the treatment of COVID-19.
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Objective: To establish a quantitative analysis model for online monitoring of the blending uniformity of hydroxychloroquine sulfate raw and auxiliary materials, so as to accurately and quickly determine the blending endpoint. Methods: A mixture of excipients and hydroxychloroquine sulfate raw material was prepared with a labeling percentage of 70%-130%. The near-infrared spectrum was collected; and the standard normal variate transformation and frst derivative by Norris smoothing were used for spectra pretreating, with 8 372-9 045 cm-1, 5 616-6 058 cm 1 used as the spectral bands. A quantitative analysis model was developed using partial least squares regression. The quantitative analysis model was used to predict the labeling percentage of hydroxychloroquine sulfate in the blending process of raw and auxiliary materials, and the blending endpoint was verified by high-performance liquid chromatography (HPLC) analysis. Results: Five primary factors were used to establish the model. The root mean square error of calibration was 0.96 and the correlation coefficient of calibration set (Rc) was 0.998. The root mean square error of prediction was 0.97 and the correlation coefficient of validation set (Rp) was 0.998. The root mean square error of cross-validation was 1.56 and the correlation coefficient of cross-validation (Rcv) was 0.995. The prediction results of the near-infrared model was consistent with the results of HPLC verification. Conclusion: The near-infrared model in this study can be used for online quantitative analysis of the blending uniformity of hydroxychloroquine sulfate, and it can accurately and quickly determine the blending endpoint.
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Objective To investigate the effect of glucosidorum tripterygll totorum combined with prednisone acetate and hydroxychloroquine sulfate in the treatment of systemic lupus erythematosus (SLE). Me thods Eighty-two patients with SLE were divided into the control group (n=41) and the observation group (n=41) by the random number table method. The control group was treated with prednisone acetate combined with hydroxychloroquine sulfate. On the basis of treatment for the control group, the observation group was treated with glucosidorum tripterygll totorum. Four weeks was taken as 1 course of treatment and they were given 3 courses of treatment. Curative effect and adverse drug reactions were evaluated. The SLE disease activity index score was to evaluate the degree of lupus before and after treatment. The levels of blood lipid indexes [triglycerides (TG), total cholesterol (TC), high density lipoprotein cholesterol (HDL-C), low density lipoprotein cholesterol (LDL-C) ], complement C3, immunoglobulin G (Ig G), anti-double stranded DNA (ds-DNA), interleukin 8 (IL-8) and interleukin 10 (IL-10) were determined. Re s ults The effective rate of the observation group was higher than that of the control group (92.50％ vs 73.17％ ), P ＜ 0.05. After treatment, the SLE-DAI score, levels of TC, TG, LDL-C, Ig G, anti-ds-DNA, IL-10 and IL-8 in the observation group were lower than those in the control group while levels of HDL-C and complement C3 were higher than those in the control group (all P ＜ 0.05). There was no significant difference in the incidence of adverse drug reactions between the two groups (56.10％ vs 43.90％ ), P＞ 0.05. Conclusion The application of glucosidorum tripterygll totorum combined with prednisone acetate and hydroxychloroquine sulfate in the treatment of SLE can reduce the inflammatory and blood lipid levels and regulate immune mechanism. The effect is exact and patients can tolerate.
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Objective:To establish a rapid HPLC testing method for chloroquine phosphate,hydroxychloroquine sulfate and amodiaquine hydrochloride.Methods:The chromatographic separation was performed on a GRACE prevail C18(53 mm×7 mm,3 μm)column,and the column temperature was maintained at 30℃.Acetonitrile-0.3% triethylamine acetonitrile solution (adjusting pH to 3.0 with phosphoric acid) (12∶88) was used as the mobile phase,the flow rate was 1.0 ml· min-1 and the UV detection wavelength was 254 nm.The qualitative research was performed using relative retention time and spectral similarity as the double indicators.The relative correction factor in the quantification analysis was used for the content determination.Results:Three anti-malarial drugs showed good behavior in one chromatographic system.The rapid HPLC testing analysis could be achieved.The qualitative research was more accurate by using the double indicators (UV spectral similarity and relative capacity factor).The HPLC qualitative accuracy was increased.The relative correction factor method for the quantification could effectively reduce the use of reference substances and speed up the analysis of HPLC.Conclusion:The method is rapid and simple,and suitable for the rapid determination of drugs.
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Objective To observe the therapeutic effect of Ziyin Yangxue Qingre Formula (Formula for enriching yin,nourishing blood and clearing heat) on primary Sjogren's Syndrome (pSS).Methods Totally 64 female pSS patients were randomized into a treating group (33 cases),and a control group (31 cases).The control group was administered Hydroxychloroquine Sulfate Tablet.In addition,the treating group was prescribed Ziyin Yangxue Qingre Formula.Three-month treatment was as one course.After one course of treatment,the changes in symptom scores,salivation quantity,tear quantity,and immuno-infective indices were observed to compare the effect between both groups.Results The total effective rate of the treating group(87.88%) was significantly higher than that (64.52%) of the control group (P